Histamine H1 receptor ligands activate ERK1/2 pathway and modulate the transcription of pro-inflammatory genes

RIPOLL, SONIA; MONCZOR, FEDERICO; ZAPPIA, C. DANIEL; SHAYO, CARINA; BURGHI, VALERIA; ECHEVERRIA, EMILIANA; FERNANDEZ, NATALIA; RIPOLL, SONIA; MONCZOR, FEDERICO; ZAPPIA, C. DANIEL; SHAYO, CARINA; BURGHI, VALERIA; ECHEVERRIA, EMILIANA; FERNANDEZ, NATALIA

Mar del Plata

Congreso; LXIV Reunión Anual de la Sociedad Argentina de Investigación Clínica (SAIC); 2019

Sociedad Argentina de Investigación Clínica (SAIC)

Recently, we showed that widely used histamine H1 receptor (H1R) ligands that exert therapeutic actions by blocking the effects of histamine (HA), display positive efficacy concerning receptor desensitization and/or internalization. Now we aimed to investigate whether these processes affect the modulation of pro-inflammatory genes and its relationship with the activation of other signaling pathways independent from G protein. While 3 h (long term) exposure to antihistamines decreased expression of pro-inflammatory genes, when we exposed A549 cells, endogenously expressing H1R to HA, chlorpheniramine (CHLOR) or diphenhydramine (DIPH) for 10 min and ligands were removed, ciclooxigenase 2 (COX-2) and interleukin 8 (IL-8) mRNA levels were increased after 2 h 50 min (among 40 and 100% for all ligands, P